HRP20110498T1 - Azetidini kao inhibitori mek za liječenje proliferativnih bolesti - Google Patents

Azetidini kao inhibitori mek za liječenje proliferativnih bolesti Download PDF

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HRP20110498T1
HRP20110498T1 HR20110498T HRP20110498T HRP20110498T1 HR P20110498 T1 HRP20110498 T1 HR P20110498T1 HR 20110498 T HR20110498 T HR 20110498T HR P20110498 T HRP20110498 T HR P20110498T HR P20110498 T1 HRP20110498 T1 HR P20110498T1
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heteroaryl
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heterocycloalkyl
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Aay Naing
Kumar Anand Neel
Joseph Bowles Owen
Bussenius Joerg
Costanzo Simona
Kimo Curtis Jeffry
Dubenko Larisa
Abhijit Joshi Anagha
R. Kennedy Abigail
Inyoung Kim Angie
Koltun Elena
Limun Manalo Jean-Claire
J. Peto Csaba
D. Rice Kenneth
H. Tsang Tsze
Charles Defina Steven
M. Blazey Charles
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Exelixis
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Abstract

Spoj formule I: ili pojedinačni stereoizomer ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat, naznačen time što su A, X, R1, R2, R3, R4, R5, R6 i R7 kako je definirano za grupu A, grupu B, grupu C ili grupu D: Grupa A: A je arilen po izboru supstituiran s jednom, dvije, tri ili četiri skupine izabrane između R10, R12, R14 iR16 gdje su R1O, R12, R14 i R16 nezavisno jedan od drugog vodik, alkil, alkenil, alkinil, halogen, halogenalkoksi, hidroksi, alkoksi, amino, alkilamino, dialkilamino, halogenalkil, -NHS(O)2R8, -CN, -C(O)R8, -C(O)OR8, -C(O)NR8R8' i -NR8C(O)R8'; X je alkil, halogen, halogenalkil ili halogenalkoksi; R1, R2, R3, R4, R5 i R6 su nezavisno vodik, halogen, nitro, NR8R8', -OR8, -NHS(O)2R8, -CN, -S(O)mR8,

Claims (43)

1. Spoj formule I: [image] ili pojedinačni stereoizomer ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat, naznačen time što su A, X, R1, R2, R3, R4, R5, R6 i R7 kako je definirano za grupu A, grupu B, grupu C ili grupu D: Grupa A: A je arilen po izboru supstituiran s jednom, dvije, tri ili četiri skupine izabrane između R10, R12, R14 iR16 gdje su R1O, R12, R14i R16 nezavisno jedan od drugog vodik, alkil, alkenil, alkinil, halogen, halogenalkoksi, hidroksi, alkoksi, amino, alkilamino, dialkilamino, halogenalkil, -NHS(O)2R8, -CN, -C(O)R8, -C(O)OR8, -C(O)NR8R8' i -NR8C(O)R8'; X je alkil, halogen, halogenalkil ili halogenalkoksi; R1, R2, R3, R4, R5 i R6 su nezavisno vodik, halogen, nitro, NR8R8', -OR8, -NHS(O)2R8, -CN, -S(O)mR8, -S(O)2NR8R8', -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)NR8'R8", -NR8C(O)OR8', -NR8C(O)R8', -CH2N(R25)(NR25aR25b), -CH2NR25C(=NH)(NR25aR25b),-CH2NR25C(=NH)(N(R25)(NO2)), -CH2NR25C(=NH)(N(R25a)(CN)),-CH2NR25C(=NH)(R25), -CH2NR25C(NR25aR25b)=CH(NO2), alkil, alkenil, alkinil, cikloalkil, heteroaril ili heterocikloalkil; gdje su alkil, alkenil, alkinil, cikloalkil, heteroaril i heterocikloalkil nezavisno po izboru supstituirani s jednom. dvije, tri, četiri, pet, šest ili sedam skupina nezavisno izabranih između halogena, alkil, halogenalkil, nitro, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilaikil, po izboru supstituirani heteroaril, -OR8, -NR8R8', -NR8S(O)2R9, -CN, -S(O)mR9, -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)NR8'R8",-NR8C(O)OR8' i -NR8C(O)R8'; ili jedan od R1 i R2 zajedno s ugljikom na koji su spojeni, R3 i R4 zajedno s ugljikom na koji su spojeni, i R5 i R6 zajedno s ugljikom na koji su spojeni čine C(O) ili C(=NOH); m je 0, 1 ili 2; R7 je vodik, halogen ili alkil; R8, R8' i R8'' su nezavisno izabrani između vodika, hidroksi, po izboru supstituirani alkoksi, alkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil; gdje alkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil su nezavisno po izboru supstituiran s jednom, dvije, tri, četiri ili pet skupina nezavisno izabranih između alkil, halogen, hidroksi, hidroksialkil, po izboru supstituirani alkoksi, alkoksialkil, halogenalkil, karboksi, alkoksikarbonil, alkeniloksikarbonil, po izboru supstituirani cikloalkil, po izboru supstituirani cikloalkiloksikarbonil, po izboru supstituirani aril, po izboru supstituirani ariloksi, po izboru supstituirani ariloksikarbonil, po izboru supstituirani arilaikii, po izboru supstituirani arilalkiloksi, po izboru supstituirani arilalkiloksikarbonil, nitro, cijano, po izboru supstituirani heterocikloalkil, po izboru supstituirani heteroaril, -S(O)nR31 (gdje n je 0, 1 ili 2 i R31 je po izboru supstituirani alkil, po izboru supstituirani aril, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), -NR34SO2R34a (gdje R34 je vodik ili alkil i R34a je alkil, alkenil, cikloalkil, aril, heteroaril ili heterocikloalkil), -SO2NR35R35a (gdje R35 je vodik ili alkil i R35a je alkil, alkenil, cikloalkil, aril, heteroaril ili heterocikloalkil), -NR32C(O)R32a (gdje R32 je vodik ili alkil i R32a je alkil, alkenil, alkoksi ili cikloalkil), -NR30R30' (gdje R30 i R30' su nezavisno vodik, alkil ili hidroksialkil), i -C(O)NR33R33a(gdje R33 je vodik ili alkil i R33a je alkil, alkenil, alkinil ili cikloalkil); i R9 je alkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil; gdje alkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil su nezavisno po izboru supstituirani jednom, dvije, tri, četiri ili pet skupina izabranih između halogena, hidroksi, alkil, halogenalkil, halogenalkoksi, amino, alkilamino, i dialkilamino; R25i R25b su nezavisno vodik, alkil, alkenil, po izboru supstituirani cikloalkil ili po izboru supstituirani aril; i R25a je vodik, alkil ili alkenil; Grupa B: A je heteroarilen po izboru supstituiran s jednom, dvije, tri ili četiri skupine izabrane između R10, R12, R14, R16 i R19 gdje R10, R12, R14i R16 su nezavisno vodik, alkil, alkenil, alkinil, halogen, halogenalkoksi, hidroksi, alkoksi, cijano, amino, alkilamino, dialkilamino, halogenalkil, alkilsulfonilamino, alkilkarbonil, alkenilkarbonil, alkoksikarbonil, alkeniloksikarbonil, aminokarbonil, alkilaminokarbonil, dialkilaminokarbonil ili alkilkarbonilamino; gdje R19 je vodik, alkil ili alkenil; i gdje je svaki alkil i alkenil, sam ili kao dio druge skupine unutar R10, R12, R14, R16, i R19 nezavisno po izboru supstituiran s halogenom, hidroksi ili alkoksi; X je alkil, halogen, halogenalkil ili halogenalkoksi; R1, R2, R3, R4, R5 i R6 su nezavisno vodik, halogen, nitro, -NR8R8', -OR8, -NHS(O)2R8, -CN, -S(O)mR8, -S(O)2NR8R8', -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)NR8'R8", -NR8C(O)OR8', -NR8C(O)R8', alkil, alkenil, alkinil, cikloalkil, heteroaril ili heterocikloalkil, gdje su alkil, alkenil, alkinil, cikloalkil, heteroaril, i heterocikloalkil nezavisno po izboru supstituirani s jednom, dvije, tri, četiri, pet, šest ili sedam skupina nezavisno izabranih između halogen, alkil, halogenalkil, nitro, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilaikil, po izboru supstituirani heteroaril, -OR8, -NR8R8', -NR8S(O)2R9, -CN, -S(O)mR9, -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)NR8'R8", -NR8C(O)OR8' i -NR8C(O)R8'; ili jedan od R1 i R2 zajedno s ugljikom na koji su spojeni, R3 i R4 zajedno s ugljikom na koji su spojeni, i R5 i R6 zajedno s ugljikom na koji su spojeni čine C(O) ili C(=NOH); m je 1 ili 2; R7 je vodik, halogen ili alkil; i R8, R8' i R8" su nezavisno izabrani između vodika, hidroksi, po izboru supstituirani alkoksi, alkil, halogenalkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil, gdje su alkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil nezavisno po izboru supstituiran s jednom, dvije, tri, četiri ili pet skupina nezavisno izabranih između alkil, halogen, hidroksi, hidroksialkil, po izboru supstituirani alkoksi, alkoksialkil, halogenalkil, karboksi, karboksi ester, nitro, cijano, -S(O)nR31 (gdje n je 0, 1 ili 2 i R31 je po izboru supstituirani alkil, po izboru supstituirani aril, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), -NR36S(O)2R36a (gdje R36 je vodik, alkil ili alkenil i R36a je alkil, alkenil, po izboru supstituirani aril, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), -S(O)2NR37R37a (gdje R37 je vodik, alkil ili alkenil i R37a je alkil, alkenil, po izboru supstituirani aril, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilalkil, po izboru supstituirani ariloksi. do izboru supstituirani arilalkiloksi, po izboru supstituirani heteroaril, -NHC(O)R32 (gdje R32 je alkil, alkenil, alkoksi ili cikloalkil) i -NR30R30' (gdje R30 i R30' su nezavisno vodik, alkil ili hidroksialkil), i -C(O)NHR33 (gdje R33 je alkil, alkenil, alkinil ili cikloalkil); Grupa C: [image] gdje je R10 vodik, alkil, alkenil, alkinil, halogen, halogenalkoksi, hidroksi, alkoksi, amino, alkilamino, dialkilamino, halogenalkil, -NHS(O)2R8, -CN, -C(O)R8, -C(O)OR8, -C(O)NR8R8' i -NR8C(O)R8'; R10a je vodik, alkil ili alkenil; Y1 je =CH- ili =N-; X je alkil, halogen, halogenalkil ili halogenalkoksi; R1, R2, R3, R4, R5 i R6 su nezavisno vodik, halogen, nitro, -NR8R8', -OR8, -NHS(O)2R8, -CN, -S(O)mR8, -S(O)2NR8R8', -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)NR8'R8", -NR8C(O)OR8', -NR8C(O)R8', alkil, alkenil, alkinil, cikloalkil, heteroaril ili heterocikloalkil, gdje su alkil, alkenil, alkinil, cikloalkil, heteroaril, i heterocikloalkil nezavisno po izboru supstituirani s jednom, dvije, tri, četiri, pet, šest ili sedam skupina nezavisno izabranih između halogen, alkil, halogenalkil, nitro, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilalkil, po izboru supstituirani heteroaril, -OR8, -NR8R8', -NR8S(O)2R9, -CN, -S(O)mR9, -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)NR8'R8", -NR8C(O)OR8' i -NR8C(O)R8'; ili jedan od R1 i R2 zajedno s ugljikom na koji su spojeni, R3 i R4 zajedno s ugljikom na koji su spojeni, i R5 i R6 zajedno s ugljikom na koji su spojeni čine C(O) ili C(=NOH); m je 1 ili 2; R7 je vodik, halogen ili alkil; i R8, R8' i R8'' su nezavisno izabrani između vodika, hidroksi, po izboru supstituirani alkoksi, alkil, halogenalkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil, gdje su alkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil nezavisno po izboru supstituirani s jednom, dvije, tri, četiri ili pet skupina nezavisno izabranih između alkil, halogen, hidroksi, hidroksialkil, po izboru supstituirani alkoksi, alkoksialkil, halogenalkil, karboksi, karboksi ester, nitro, cijano, -S(O)nR31 (gdje n je 0, 1 ili 2 i R31 je po izboru supstituirani alkil, po izboru supstituirani aril, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), -NR36S(O)2R36a (gdje R36 je vodik, alkil ili alkenil i R36a je alkil, alkenil, po izboru supstituirani aril, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), -S(O)2NR37R37a (gdje R37 je vodik, alkil ili alkenil i R37a je alkil, alkenil, po izboru supstituirani aril, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilalkil, po izboru supstituirani ariloksi, po izboru supstituirani arilalkiloksi, po izboru supstituirani heteroaril, -NHC(O)R32 (gdje R32 je alkil, alkenil, alkoksi ili cikloalkil) i -NR30R30' (gdje R30 i R30' su nezavisno vodik, alkil ili hidroksialkil), i -C(O)NHR33 (gdje R33 je alkil, alkenil, alkinil ili cikloalkil); ili Grupa D: A e [image] R40 i R40a su nezavisno vodik ili alkil; X je alkil, halogen, halogenalkil ili halogenalkoksi; R1, R2, R3, R4, R5 i R6 su nezavisno vodik, halogen, nitro, -NR8R8', -OR8, -NHS(O)2R8, -CN, -S(O)mR8, -S(O)2NR8R8', -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)NR8'R8", -NR8C(O)OR8', -NR8C(O)R8', alkil, alkenil, alkinil, cikloalkil, heteroaril ili heterocikloalkil, gdje su alkil, alkenil, alkinil, cikloalkil, heteroaril, i heterocikloalkil nezavisno po izboru supstituirani s jednom, dvije, tri, četiri, pet, šest ili sedam skupina nezavisno izabranih između halogen, alkil, halogenalkil, nitro, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilaikil, po izboru supstituirani heteroaril, -OR8, -NR8R8', -NR8S(O)2R9, -CN, -S(O)mR9, -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)NR8'R8", -NR8C(O)OR8' i -NR8C(O)R8'; ili jedan od R1 i R2 zajedno s ugljikom na koji su spojeni, R3 i R4 zajedno s ugljikom na koji su spojeni, i R5 i R6 zajedno s ugljikom na koji su spojeni čine C(O) ili C(=NOH); m je 1 ili 2; R7 je vodik, halogen ili alkil; i R8, R8' i R8'' su nezavisno izabrani između vodik, hidroksi, po izboru supstituirani alkoksi, alkil, halogenalkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil, gdje su alkil, alkenil, alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil nezavisno po izboru supstituiran s jednom, dvije, tri, četiri ili pet skupina nezavisno izabranih između alkil, halogen, hidroksi, hidroksialkil, po izboru supstituirani alkoksi, alkoksialkil, halogenalkil, karboksi, karboksi ester, nitro, cijano, -S(O)nR31 (gdje n je 0, 1 ili 2 i R31 je po izboru supstituirani alkil, po izboru supstituirani aril, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), -NR36S(O)2R36a (gdje R36 je vodik, alkil ili alkenil i R36a je alkil, alkenil, po izboru supstituirani aril, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), -S(O)2NR37R37a (gdje R37 je vodik, alkil ili alkenil i R37a je alkil, alkenil, po izboru supstituirani aril, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil ili po izboru supstituirani heteroaril), po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilaikil, po izboru supstituirani ariloksi, po izboru supstituirani arilalkiloksi, po izboru supstituirani heteroaril, -NHC(O)R32 (gdje R32 je alkil, alkenil, alkoksi ili cikloalkil) i -NR30R30' (gdje R30 i R30' su nezavisno vodik, alkil ili hidroksialkil), i -C(O)NHR33 (gdje R33 je alkil, alkenil, alkinil ili cikloalkil).
2. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A, Grupe B i Grupe C gdje Grupa A A je fenilen po izboru supstituiran s jednom ili dvije skupine izabrane između R10, R12, R14 i R16 gdje R10, R12, R14 i R16 su nezavisno vodik ili halogen; X je halogen; R1, R2, R5i R6 su vodik; R3 je vodik, halogen, hidroksi, alkoksi ili amino; R4 je vodik, -NR8R8', -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)R8', -CH2N(R25)(NR25aR25b), -CH2NR25C(=NH)(NR25aR25b), -CH2NR25C(=NH)(N(R25a)(NO2)), -CH2NR25C(=NH)(N(R25a)(CN)), -CH2NR25C(=NH)(R25), -CH2NR25C(NR25aR25b)=CH(NO2), alkil, alkenil, cikloalkil, heterocikloalkil ili heteroaril; gdje je alkil po izboru supstituiran jednom, dvije ili tri skupine nezavisno izabrane između -OR8, halogen, nitro, -S(O)mR9, po izboru supstituirani heterocikloalkil, -NR8R8', -NR8C(O)R8', -NR8S(O)2R9, -NR8C(O)OR8', i aril; gdje je cikloalkil po izboru supstituiran jednom ili dvije skupine izabrane između -OR8 i -NR8R8'; gdje je heterocikloalkil po izboru supstituiran s jednom ili dvije skupine nezavisno izabrane između alkil i -C(O)OR8; i gdje je heteroaril po izboru supstituiran s _NR8R8'; ili R3 i R4 zajedno s ugljikom na koji su spojeni čine C(O) ili C(=NOH); m je 0; R7je halogen; R8 i R8' su nezavisno izabrani između vodik, hidroksi, alkil, alkenil, alkinil, aril, heterocikloalkil, heteroaril, i cikloalkil; gdje su R8 i R8' alkil nezavisno po izboru supstituiran s jednom, dvije ili tri skupine nezavisno izabrane između hidroksi, -NR30R30' (gdje R30 i R30 su nezavisno vodik, alkil ili hidroksialkil), po izboru supstituirani heteroaril, po izboru supstituirani cikloalkil), po izboru supstituirani alkoksi, po izboru supstituirani cikloalkil, po izboru supstituirani aril, po izboru supstituirani heterocikloalkil, po izboru supstituirani heteroaril, -C(O)NR33R33a (gdje R33 je vodik ili alkil i R33a je alkil, alkenil, alkinil ili cikloalkil), po izboru supstituirani ariloksi, -S(O)nR31 (gdje n je O i R31 je alkii), karboksi, alkoksikarbonil, i _NR32C(O)R32a (gdje R32 je vodik ili alkil i R32a je alkil, alkenil, alkoksi ili cikloalkil); ili gdje alkil je po izboru supstituiran s jednim, dva, tri, četiri ili pet halogena; gdje su R8 i R8' heteroaril nezavisno po izboru supstituiran s jednom ili dvije skupine nezavisno izabrane između amino i alkil; gdje su R8 i R8' heterocikloalkil nezavisno po izboru supstituiran s jednom, dvije ili tri skupine nezavisno izabrane između alkil, alkoksikarbonil, po izboru supstituirani arilaikii, hidroksi, alkoksi, i hidroksialkil; gdje su R8 i R8'aril nezavisno po izboru supstituiran s jednom ili dvije skupine nezavisno izabrane između hidroksi, alkoksi, halogen, -NR32C(O)R32a (gdje R32 je vodik ili alkil i R32a je alkil, alkenil, alkoksi ili cikloalkil), i -NR34SO2R34a (gdje R34 je vodik ili alkil i R34a je alkil, alkenil, cikloalkil, aril, heteroaril ili heterocikloalkil); i gdje su R8 i R8' cikloalkil nezavisno po izboru supstituiran s jednom, dvije ili tri skupine nezavisno izabrane između hidroksi, hidroksialkil, alkoksi, karboksi, -C(O)NR33R33a (gdje R33 je vodik ili alkil i R33a je alkil, alkenil, alkinil ili cikloalkil), i po izboru supstituirani cikloalkil; i R9 je alkil ili aril; Grupa B A je tien-3,4-diil, benzo[d]izoksazol-5,6-diil, 1H-indazol-5,6-diil (po izboru supstituirani na N1 položaju s R19 gdje R19 je alkil ili alkenil), benzo[d]oksazol-5,6-diil, 1H-benzo[d]imidazol-5,6-diil (po izboru supstituirani na N1 položaju s R19 gdje R19 je alkil ili alkenil), 1H-benzo[d][1,2,3]triazol-5,6-diil (po izboru supstituirani na N1 položaju s R19 gdje R19 je alkil ili alkenil), imidazo[1,2-a]piridin-6,7-diil, cinnolin-6,7-diil, kinolin-6,7-diil, piridin-3,4-diil, 1-oksido-piridin-3,4-diil, [1,2,4]triazolo[4,3-a]piridin-6,7-diil ili 2,3-dihidroimidazo[1,2-a]piridin-6,7-diil; gdje A je po izboru supstituiran s jednom, dvije ili tri skupine nezavisno izabrane između R10, R12, R14, R16 i R19 gdje R10, R12, R14i R16 su nezavisno vodik, alkil, halogen ili amino; i R19 je vodik ili alkil; X je halogen; R1, R2, R5 i R6 su vodik; R3je vodik ili hidroksi; R4 je -NR8R8', heterocikloalkil, heteroaril ili alkil; gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; R7je halogen; R8 je vodik ili alkil; i R8'je vodik, alkil ili cikloalkil; gdje cikloalkil je po izboru supstituiran s jednom ili dvije skupine nezavisno izabrane između hidroksi i alkil; Grupa C A je [image] R10 je vodik ili halogen; R10a je vodik ili alkil; Y1 je =CH- ili =N-; X je halogen; R1, R2, R5i R6 su vodik; R3 je vodik ili hidroksi; R4 je -NR8R8', heterocikloalkil, heteroaril ili alkil; gdje alkil je po izboru supstituiran s -NR8R8' i gdje heteroaril je po izboru supstituiran s alkilom; R7je halogen; R8 je vodik ili alkil; i R8' je vodik, alkil ili cikloalkil; gdje cikloalkil je po izboru supstituiran s jednom ili dvije skupine nezavisno izabrane između hidroksi i alkil; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
3. Spoj prema zahtjevu 1, naznačen time što je R3 halogen, nitro, -NR8R8', -OR8, -NHS(O)2R8, -CN, -S(O)mR8, -S(O)2NR8R8', -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)NR8'R8", -NR8C(O)OR8', -NR8C(O)R8', -CH2N(R25)(NR25aR25b), -CH2NR25C(=NH)(NR25aR25b), -CH2NR25C(=NH)(N(R25a)(NO2)), -CH2NR25C(=NH)(N(R25a)(CN)), -CH2NR25C(=NH)(R25), -CH2NR25C(NR25aR25b)=CH(NO2), alkil, alkenil, alkinil, cikloalkil, heteroaril ili heterocikloalkil; gdje alkil, alkenil, alkinil, cikloalkil, heteroaril, i heterocikloalkil su nezavisno po izboru supstituirani s jednom, dvije, tri, četiri, pet, šest ili sedam skupina nezavisno izabranih između halogen, alkil, halogenalkil, nitro, po. izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilaikii, po izboru supstituirani heteroaril, po izboru supstituirani heteroarilalkil, -OR8, -NR8R8', -NR8S(O)2R9, -CN, -S(O)mR9, -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)NR8'R8", -NR8C(O)OR8' i -NR8C(O)R8'; i R4 je kako je defniran u zahtjevu 1; ili R3 i R4 zajedno s ugljikom na koji su spojeni čine C(O) ili C(=NOH); ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
4. Spoj prema zahtjevu 1, naznačen time što R3 i R4 su nezavisno halogen, nitro, -NR8R8', -OR8, -NHS(O)2R8, -CN, -S(O)mR8, -S(O)2NR8R8', -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)NR8'R8", -NR8C(O)OR8', -NR8C(O)R8', -CH2N(R25)(NR25aR25b), -CH2NR25C(=NH)(NR25aR25b), -CH2NR25C(=NH)(N(R25a)(NO2)), -CH2NR25C(=NH)(N(R25a)(CN)), -CH2NR25C(=NH)(R25), -CH2NR25C(NR25aR25b)=CH(NO2), alkil, alkenil, alkinil, cikloalkil, heteroaril ili heterocikloalkil; gdje alkil, alkenil, alkinil, cikloalkil, heteroaril, i heterocikloalkil su nezavisno po izboru supstituirani s jednom, dvije, tri, četiri, pet, šest ili sedam skupina nezavisno izabranih između halogen, alkil, halogenalkil, nitro, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilaikil, po izboru supstituirani heteroaril, po izboru supstituirani heteroarilalkil, -OR8, -NR8R8', -NR8S(O)2R9, -CN, -S(O)mR9, -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)NR8'R8", -NR8C(O)OR8' i -NR8C(O)R8'; ili R3 i R4 zajedno s ugljikom na koji su spojeni čine C(O) ili C(=NOH); ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
5. Spoj prema zahtjevu 1, naznačen time što R7 je halogen; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
6. Spoj prema zahtjevu 1, naznačen time što X je halogen; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
7. Spoj prema zahtjevu 1, naznačen time što R1, R2, R5 i R6 su vodik; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
8. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A gdje A je fenilen; i R4 je -NR8R8' (gdje R8 je vodik, hidroksi, alkil, alkoksi, aril, cikloalkil, heteroaril ili heterocikloalkil i R8' je hidroksi, alkoksi, aril, cikloalkil, heteroaril ili heterocikloalkil), -NHS(O)2R8, -CN, -S(O)mR8, -S(O)2NR8R8', -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)NR8'R8", -NR8C(O)OR8', -NR8C(O)R8', -CH2N(R25)(NR25aR25b), -CH2NR25C(=NH)(NR25aR25b), -CH2NR25C(=NH)(N(R25a)(NO2)), -CH2NR25C(=NH)(N(R25a)(CN)), -CH2NR25C(=NH)(R25), -CH2NR25C(NR25aR25b)=CH(NO2), alkenil ili alkinil; gdje su alkenil i alkinil po izboru supstituirani s jednom, dvije, tri, četiri, pet, šest ili sedam skupina nezavisno izabranih između halogen, alkil, halogenalkil, nitro, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilaikii, po izboru supstituirani heteroaril, po izboru supstituirani heteroarilalkil, -OR8, -NR8R8', -NR8S(O)2R9, -CN, -S(O)mR9, -C(O)R8, -C(O)OR8, -C(O)NR8R8',-NR8C(O)NR8'R8", -NR8C(O)OR8' i -NR8C(O)R8'; ili R3 i R4 zajedno s ugljikom na koji su spojeni čine C(O) ili C(=NOH); ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
9. Spoj prema zahtjevu 1, naznačen time što R3 je vodik, halogen, hidroksi, amino ili alkoksi; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
10. Spoj prema zahtjevu 1, naznačen time što R4 je vodik, -NR8R8', -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)R8', -CH2N(R25)(NR25aR25b), -CH2NR25C(=NH)(NR25aR25b), -CH2NR25C(=NH)(N(R25a)(NO2)), -CH2NR25C(=NH)(N(R25a)(CN)), -CH2NR25C(=NH)(R25), -CH2NR25C(NR25aR25b)=CH(NO2), alkil, alkenil, cikloalkil, heterocikloalkil ili heteroaril; gdje je alkil po izboru supstituiran s jednom, dvije ili tri -OR8, halogen, nitro, -S(O)mR9, po izboru supstituirani heterocikloalkil, -NR8R8', -NR8C(O)R8', -NR8S(O)2R9, -NR8C(O)OR8', aril; gdje je cikloalkil po izboru supstituiran s jednom ili dvije -NR8R8'; gdje heterocikloalkil je po izboru supstituiran s jednom ili dvije skupine nezavisno izabrane između alkil i -C(O)OR8; i gdje je heteroaril po izboru supstituiran s -NR8R8'; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
11. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A gdje A je fenilen po izboru supstituiran s jednom ili dvije skupine nezavisno izabrane između R10, R12, R14 i R16 gdje R10, R12, R14 i R16 su nezavisno vodik ili halogen; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
12. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A gdje A je fenilen; R3 je vodik; i R4 je vodik, -NR8R8', -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)R8', alkil ili heterocikloalkil; gdje je alkil po izboru supstituiran s jednom ili dvije skupine nezavisno izabrane između -OR8 i -NR8R8'; i gdje heterocikloalkil je po izboru supstituiran s -NR8R8'; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
13. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A gdje A je fenilen; R3 je alkoksi; i R4 je alkil ili heterocikloalkil gdje je alkil supstituiran s -NR8R8'; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
14. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A gdje A je fenilen; R3 je halogen; i R4 je alkil ili heterocikloalkil gdje je alkil supstituiran s -NR8R8'; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
15. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A gdje A je fenilen i R3 i R4 zajedno s ugljikom na koji su spojeni čine C(O) ili C(=NOH); ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
16. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A gdje A je fenilen; R3 je hidroksi; i R4 je vodik, -C(O)NR8R8', -CH2N(R25)(NR25aR25b), -CH2NR25C(=NH)(NR25aR25b), -CH2NR25C(=NH)(N(R25a)(NO2)), -CH2NR25C(=NH)(N(R25a)(CN)), -CH2NR25C(=NH)(R25), -CH2NR25C(NR25aR25b)=CH(NO2), alkil, alkenil, heterocikloalkil, cikloalkil, heterocikloalkil ili heteroaril; gdje je alkil po izboru supstituiran s jednom, dvije ili tri skupine izabrane između -OR8, halogen, nitro, -S(O)mR9, po izboru supstituirani heterocikloalkil, -NR8R8', -NR8C(O)R8', po izboru supstituirani heteroaril, -NR8S(O)2R9, -NR8C(O)OR8', i aril; gdje cikloalkil je po izboru supstituiran s jednom ili dvije skupine nezavisno izabrane između -NR8R8' i -C(O)NR33R33a; gdje heterocikloalkil je po izboru supstituiran s jednom, dvije ili tri skupine nezavisno izabrane između alkil i -C(O)OR8; i gdje heteroaril je po izboru supstituiran s -NR8R8'; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
17. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A gdje A je fenilen; R7 je jod ili brom; X je fluor ili klor; i R1, R2, R5 i R6 su vodik; i R10, R12, R14 i R16 su nezavisno vodik ili fluor; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
18. Spoj prema zahtjevu 17, naznačen time što R10 je 3-fluor i R12, R14 i R16 su vodik ili halogen; R10 je 3-fluor, R12 je 4-fluor, i R14 i R16 su vodik; R10 je 4-fluor, R12 je 5-fluor, i R14 i R16 su vodik; R10 je 4-fluor, R12 je 6-fluor, i R14 i R16 su vodik; ili R12 je 4-fluor i R10, R14, i R16 su vodik; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
19. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe A gdje A je fenilen i R3je hidroksi; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
20. Spoj prema zahtjevu 19, naznačen time što R4 je -C(O)NR8R8', -CH2N(R2S)(NR25aR25b), -CH2NR25C(=NH)(NR25aR25b), -CH2NR25C(=NH)(N(R25a)(NO2)), -CH2NR25C(=NH)(N(R25a)(CN)), -CH2NR25C(=NH)(R25), -CH2NR25C(NR25aR25b)=CH(NO2), alkil, cikloalkil, heterocikloalkil ili heteroaril; gdje su alkil, cikloalkil, heteroaril, i heterocikloalkil nezavisno po izboru supstituirani s jednom, dvije, tri ili četiri skupine nezavisno izabrane između halogena, alkil, halogenalkil, nitro, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilalkil, po izboru supstituirani heteroaril, po izboru supstituirani heteroarilalkil, -OR8, -NR8R8', -NR8S(O)2R9, -CN, -S(O)mR9, -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)NR8'R8", -NR8C(O)OR8' i -NR8C(O)R8'; ili gdje je alkil po izboru supstituiran s jednim, dva, tri, četiri, pet, šest ili sedam halogena; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
21. Spoj prema zahtjevu 20, naznačen time što R4 je alkil, heterocikloalkil ili heteroaril; gdje je alkil po izboru supstituiran s -NR8R8'; gdje heterocikloalkil je po izboru supstituiran s alkil ili -C(O)OR8; i gdje heteroaril je po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
22. Spoj prema zahtjevu 1, naznačen time što R1 je halogen, nitro, -NR8R8', -OR8, -NHS(O)2R8, -CN, -S(O)mR8, -S(O)2NR8R8', -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)OR8', -NR8C(O)NR8'R8", -NR8C(O)OR8', -NR8C(O)R8', -CH2N(R25)(NR25aR25b), -CH2NR25C(=NH)(NR25aR25b), -CH2NR25C(=NH)(N(R25a)(NO2)), -CH2NR25C(=NH)(N(R25a)(CN)), -CH2NR25C(=NH)(R25) ili -CH2NR25C(NR25aR25b)=CH(NO2), alkil, alkenil, alkinil, cikloalkil, heteroaril ili heterocikloalkil; gdje the alkil, alkenil, alkinil, cikloalkil, heteroaril ili heterocikloalkil su nezavisno po izboru supstituirani s jednom, dvije, tri, četiri, pet, šest ili sedam skupina nezavisno izabranih između halogen, alkil, halogenalkil, nitro, po izboru supstituirani cikloalkil, po izboru supstituirani heterocikloalkil, po izboru supstituirani aril, po izboru supstituirani arilaikil, po izboru supstituirani heteroaril, -OR8, -NR8R8', -NR8S(O)2R9, -CN, -S(O)mR9, -C(O)R8, -C(O)OR8, -C(O)NR8R8', -NR8C(O)NR8'R8", -NR8C(O)OR8' i -NR8C(O)R8'; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje heteroaril je po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
23. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe B gdje A je tien-3,4-diil, benzo[d]izoksazol-5,6-diil, 1H-indazol-5,6-diil (po izboru supstituirani na N1 položaju s R19 gdje R19 je alkil ili alkenil), benzo[d]oksazol-5,6-diil, 1 H-benzo[d]imidazol-5,6-diil (po izboru supstituirani na N1 položaiu s R19 gdje R19 je alkil ili alkenil), 1H-benzo[d][1,2,3]triazol-5,6-diil (po izboru supstituirani na N1 položaju s R19 gdje R19 je alkil ili alkenil), imidazo[1,2-a]piridin-6,7-diil, cinnolin-6,7-diil, kinolin-6,7-diil, piridin-3,4-diil, 1-oksido-piridin-3,4-diil, [1,2,4]triazolo[4,3-a]piridin-6,7-diil ili 2,3-dihidroimidazo[1,2-a]piridin-6,7-diil; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
24. Spoj prema zahtjevu 1, naznačen time što A je tien-3,4-diil; R10 i R12 su vodik; X i R7 su halogen; i R1, R2, R5, i R6 su vodik; ili stereoizomer tog spoja ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
25. Spoj prema zahtjevu 24, naznačen time što R3 je vodik ili hidroksi; i R4 je -NR8R8', heterocikloalkil, heteroaril ili alkil, gdje je alkil po izboru supstituiran s -NR8R8'; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
26. Spoj prema zahtjevu 1, naznačen time što je izabran između Grupe B gdje A je benzo[d]izoksazol-5,6-diil; R10, R12, i R14 su nezavisno vodik, halogen ili alkil; R1, R2, R5, i R6 su vodik; X i R7 su halogen; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje heteroaril je po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
27. Spoj prema zahtjevu 23 prema formuli I(g) ili I(h): [image] naznačen time što R10, R12 i R14 su nezavisno vodik, halogen ili alkil; R19 je alkil ili alkenil; R1, R2, R5, i R6 su vodik; X i R7 su halogen; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
28. Spoj prema zahtjevu 23 prema formuli I(i) ili 10): [image] naznačen time što R10, R12 i R14 su nezavisno vodik, halogen ili alkil; R1, R2, R5, i R6 su vodik; X i R7 su halogen; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
29. Spoj prema zahtjevu 23 prema formuli I(n) ili 1(0): [image] naznačen time što R7 je halogen ili alkil; X je halogen; R19 je alkil; R1, R2, R5, i R6 su vodik; R10, R12, i R14 su nezavisno vodik ili halogen; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
30. Spoj prema zahtjevu 23 prema formuli I(p): [image] naznačen time što R1, R2, R5, i R6 su vodik; X i R7 su halogen; R10 i R12 su nezavisno vodik, halogen ili alkil; R19 je vodik ili alkil; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
31. Spoj prema zahtjevu 23 prema formuli I(q): [image] naznačen time što R1, R2, R5, i R6 su vodik; X i R7 su halogen; R10, R12, R14, i R16 su nezavisno vodik ili halogen; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
32. Spoj prema zahtjevu 23 prema formuli I(r): [image] naznačen time što R1, R2, R5, i R6 su vodik; X i R7 su halogen; R10 i R12 su nezavisno vodik, halogen ili alkil; R14 je vodik, halogen, alkil ili amino; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
33. Spoj prema zahtjevu 23 prema formuli I(s): [image] naznačen time što R1, R2, R5, i R6 su vodik; X i R7 su halogen; R10 i R12 su nezavisno vodik, halogen ili alkil; R14 je vodik, halogen, alkil ili amino; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
34. Spoj prema zahtjevu 23 prema formuli I(u), I(v), I(w) ili I(x): [image] naznačen time što R1, R2, R5, i R6 su vodik; X i R7 su halogen; R10, R12, i R14 su nezavisno vodik, halogen ili alkil; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilorn: ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
35. Spoj prema zahtjevu 1 izabran između Grupe C i prema formuli I(y) ili I(z): [image] naznačen time što R1, R2, R5, i R6 su vodik; X i R7 su halogen; R10 je vodik, halogen ili alkil; R10a je alkil; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
36. Spoj prema zahtjevu 1 izabran između Grupe D i prema formuli I(aa) ili I(bb): [image] naznačen time što R1, R2, R5, i R6 su vodik; X i R7 su halogen; R3 je hidroksi; i R4 je heterocikloalkil, alkil ili heteroaril, gdje je alkil po izboru supstituiran s -NR8R8' i gdje je heteroaril po izboru supstituiran s alkilom; ili pojedinačni stereoizomer tog spoja ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvat.
37. Spoj prema zahtjevu 1, naznačen time što je izabran iz grupe koja obuhvaća: [image] [image] [image] [image] [image] [image] [image] [image]
38. Farmaceutska smjesa, naznačena time što sadrži spoj prema zahtjevu 1, ili njegov pojedinačni stereoizomer ili smjesu stereoizomera, ili po izboru njegovu farmaceutski prihvatljivu sol ili solvat, i farmaceutski prihvatljiv nosač, pomoćnu tvar ili punilo.
39. In vitro postupak inhibicije MEK-a u stanici, naznačen time što obuhvaća dovođenje te stanice u doticaj sa spojem prema zahtjevu 1, ili njegovim pojedinačnim stereoizomerom ili smjesom stereoizomera, ili po izboru s njegovom farmaceutski prihvatljivom soli ili solvatom, i po izboru s farmaceutski prihvatljivim nosačem, pomoćnom tvari ili punilom.
40. Spoj, njegov pojedinačni stereoizomer ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvate, prema bilo kojem od zahtjeva 1 do 37, naznačen time što je za uporabu u medicini.
41. Spoj, njegov pojedinačni stereoizomer ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvate, prema zahtjevu 40, naznačen time što je uporaba liječenje proliferativne bolesti.
42. Spoj, njegov pojedinačni stereoizomer ili smjesa stereoizomera, ili po izboru njegova farmaceutski prihvatljiva sol ili solvate, prema bilo kojem od zahtjeva 1 do 37, naznačen time što je za uporabu u liječenju raka.
43. Spoj, njegov pojedinačni stereoizomer ili smjesa stereoizomera prema zahtjevu 42, naznačen time što je rak melanom, rak kolona, rak rektuma, rak gušterače, rak dojke, rak ne-malih stanica pluća, rak malih stanica pluća, papilami i anaplastični rak štitnjače, rak endometrija ili rak jajnika.
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